Oral absorption efficiency of acid-labile antibiotics from lipid-drug delivery systems.

The utility of cholesterol, cholesteryl acetate, and beta-sitosterol in protecting and improving the oral absorption efficiency of acid-labile antibiotics is discussed. The potassium salts of penicillin G and penicillin V and erythromycin lactobionate were studied. The stability of the two penicillins in simulated gastric fluid was determined iodometrically. The rank order of acid protective activity was: cholesteryl acetate greater than beta-sitosterol greater than cholesterol. Oral administration of erythromycin lactobionate coated with cholesteryl acetate produced a twofold increase in human urinary excretion of erythromycin when compared with the uncoated material. Potassium salts of penicillin G and penicillin V coated with cholesteryl acetate yielded 1.6- and 2-fold higher urine levels, respectively, as compared with the uncoated candidates.